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Radiolabeled oligonucleotides for antisense imaging.
Current Organic Synthesis ( IF 1.8 ) Pub Date : 2011-07-31 , DOI: 10.2174/157017911796117241
Arun K Iyer 1 , Jiang He
Affiliation  

Oligonucleotides radiolabeled with isotopes emitting γ-rays (for SPECT imaging) or positrons (for PET imaging) can be useful for targeting messenger RNA (mRNA) thereby serving as non-invasive imaging tools for detection of gene expression in vivo (antisense imaging). Radiolabeled oligonucleotides may also be used for monitoring their in vivo fate, thereby helping us better understand the challenges to its delivery for antisense targeting. These developments have led to a new area of molecular imaging and targeting, utilizing radiolabeled antisense oligonucleotides. However, the success of antisense imaging relies heavily on overcoming the challenges for its targeted delivery in vivo. Furthermore, the low ability of the radiolabeled antisense oligonucleotide to subsequently internalize into the cell and hybridize with its target mRNA poses additional challenges in realizing its potentials. This review covers the advances in the antisense imaging probe development for PET and SPECT, with an emphasis on radiolabeling strategies, stability, delivery and in vivo targeting.



中文翻译:

用于反义成像的放射性标记寡核苷酸。

用发射 γ 射线(用于 SPECT 成像)或正电子(用于 PET 成像)的同位素放射性标记的寡核苷酸可用于靶向信使 RNA (mRNA),从而用作检测体内基因表达的非侵入性成像工具(反义成像)。放射性标记的寡核苷酸也可用于监测其体内命运,从而帮助我们更好地了解其反义靶向递送面临的挑战。这些发展导致了分子成像和靶向的新领域,利用放射性标记的反义寡核苷酸。然而,反义成像的成功在很大程度上取决于克服其体内靶向递送的挑战。此外,放射性标记的反义寡核苷酸随后内化到细胞中并与其目标 mRNA 杂交的能力较低,这对实现其潜力提出了额外的挑战。本综述涵盖了 PET 和 SPECT 反义成像探针开发的进展,重点是放射性标记策略、稳定性、递送和体内靶向。

更新日期:2011-07-31
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